US12552829B2ActiveUtilityA9

Compositions and methods for treating CNS disorders

Assignee: SAGE THERAPEUTICS INCPriority: Jun 27, 2019Filed: Jun 29, 2020Granted: Feb 17, 2026
Est. expiryJun 27, 2039(~12.9 yrs left)· nominal 20-yr term from priority
C07J 63/002C07J 61/00A61P 25/24A61K 31/57C07J 63/008A61P 9/00A61P 25/30A61P 25/04A61P 25/28A61P 25/14A61P 25/18A61P 25/20A61P 25/00C07J 43/003
51
PatentIndex Score
0
Cited by
63
References
75
Claims

Abstract

Provided herein is a compound of Formula I, II, IIIa, IIIb, V, VIa, VIb, VII, VIII, IX, or XI: or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of Formula I, II, IIIa, IIIb, V, VIa, VIb, VII, VIII, IX, or X, and methods of using the compounds, e.g., in the treatment of CNS-related disorders.

Claims

exact text as granted — not AI-modified
What is claimed: 
     
         1 . A compound of Formula (I): 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein
    represents a single or double bond, provided if a double bond is present, then one of R 6a  or R 6b  is absent and R 5  is absent; 
 R X  is selected from the group consisting of halo, —OH, —OR Q1 , and substituted or unsubstituted alkyl, wherein R Q1  is substituted or unsubstituted alkyl; 
 R Y  is halo or substituted or unsubstituted alkyl; or 
 R Y  and R X  may join together with the intervening atoms to form a substituted or unsubstituted carbocyclyl or a substituted or unsubstituted heterocyclyl; 
 R 3  is selected from the group consisting of substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; 
 R 5  is hydrogen or methyl; 
 each instance of R 22  is independently selected from the group consisting of halogen, —NO 2 , —CN, —OR GA , —N(R GA ) 2 , —C(═O)R GA , —C(═O)OR GA , —OC(═O)R GA , —OC(═O)OR GA , —C(═O)N(R GA ) 2 , —N(R GA )C(═O)R GA , —OC(═O)N(R GA ) 2 , —N(R GA )C(═O)OR GA , —N(R GA )C(═O)N(R GA ) 2 , —SR GA , —S(═O)R GA , —S(O) 2 R GA , —S(O) 2 OR GA , —OS(═O) 2 R GA , —S(═O) 2 N(R GA ) 2 , —N(R GA )S(═O) 2 R GA , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocylyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl, wherein each instance of R GA  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted C 3-6  carbocylyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to oxygen, and a nitrogen protecting group when attached to nitrogen, or two R GA  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclyl or heteroaryl ring; 
 each of R 1a , R 1b , R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , and R 12b  is independently selected from the group consisting of hydrogen, halogen, cyano, —NO 2 , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR A1 , —N(R A1 ) 2 , —SR A1 , —C(═O)R A1 , —C(═O)OR A1 , —C(═O)SR A1 , —C(═O)N(R A1 ) 2 , —OC(═O)R A1 , —OC(═O)OR A1 , —OC(═O)N(R A1 ) 2 , —OC(═O)SR A1 , —OS(═O) 2 R A1 , —OS(═O) 2 OR A1 , —OS(═O) 2 N(R A1 ) 2 , —N(R A1 )C(═O)R A1 , —N(R A1 )C(═NR A1 )R A1 , —N(R A1 )C(═O)OR A1 , —N(R A1 )C(═O)N(R A1 ) 2 , —N(R A1 )S(═O) 2 R A1 , —N(R A1 )C(═NR A1 )N(R A1 ) 2 , —N(R A1 )S(═O) 2 OR A1 , —N(R A1 )S(═O) 2 N(R A1 ) 2 , —SC(═O)OR A1 , —SC(═O)R A1 , —SC(═O)SR A1 , —SC(═O)N(R A1 ) 2 , —S(═O) 2 R A1 , —S(═O) 2 OR A1 , or —S(═O) 2 N(R A1 ) 2 , wherein each instance of R A1  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted C 3-6  carbocyclyl, or substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to oxygen, a nitrogen protecting group when attached to nitrogen, and a sulfur protecting group when attached to sulfur, or two R A1  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclic ring; 
 each of R 6a  and R 6b  is independently selected from the group consisting of hydrogen, halogen, cyano, —NO 2 , —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, and substituted or unsubstituted alkynyl; or R 6a  and R 6b  are joined to form an oxo (═O) group; 
 each of R 15a , R 15b , R 16a , and R 16b  is independently selected from the group consisting of hydrogen, halogen, —CN, —NO 2 , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR C3 , —N(R C3 ) 2 , —SR C3 , —C(═O)R C3 , —C(═O)OR C3 , —C(═O)SR C3 , —C(═O)N(R C3 ) 2 , —OC(═O)R C3 , —OC(═O)OR C3 , —OC(═O)N(R C3 ) 2 , —OC(═O)SR C3 , —OS(═O) 2 R C3 , —OS(═O) 2 OR C3 , —OS(═O) 2 N(R 3 ) 2 , —N(R C3 )C(═O)R C3 , —N(R C3 )C(═NR C3 )R C3 , —N(R C3 )C(═O)OR C3 , —N(R C3 )C(═O)N(R C3 ) 2 , —N(R C3 )C(═NR C3 )N(R C3 ) 2 , —N(R C3 )S(═O) 2 R C3 , —N(R C3 )S(═O) 2 OR C3 , —N(R C3 )S(═O) 2 N(R C3 ) 2 , —SC(═O)R C3 , —SC(═O)OR C3 , —SC(═O)SR C3 , —SC(═O)N(R C3 ) 2 , —S(═O) 2 R C3 , —S(═O) 2 OR C3 , or —S(═O) 2 N(R C3 ) 2 , wherein each instance of R C3  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group when attached to oxygen, a nitrogen protecting group when attached to nitrogen, and a sulfur protecting group when attached to sulfur, or two R C3  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclic ring; 
 R 19  is hydrogen or substituted or unsubstituted alkyl; 
 n is 0, 1, 2, or 3; and 
 t is 2 or 3. 
 
     
     
         2 . The compound or pharmaceutically acceptable salt of  claim 1 , wherein t is 2. 
     
     
         3 . The compound or pharmaceutically acceptable salt of  claim 2 , wherein R 3  is substituted or unsubstituted C 1-6  alkyl. 
     
     
         4 . The compound or pharmaceutically acceptable salt of  claim 3 , wherein R 3  is C 1-3  alkyl optionally substituted with C 1-3  alkoxy. 
     
     
         5 . The compound or pharmaceutically acceptable salt of  claim 4 , wherein R 3  is methyl, ethyl, propyl, n-propyl, —CH 2 OCH 3 , or —CH 2 OCH 2 CH 3 . 
     
     
         6 . The compound or pharmaceutically acceptable salt of  claim 2 , wherein R 19  is hydrogen or unsubstituted C 1-3  alkyl. 
     
     
         7 . The compound or pharmaceutically acceptable salt of  claim 2 , wherein each of R 15a  and R 15b  is independently hydrogen or substituted or unsubstituted alkyl. 
     
     
         8 . The compound or pharmaceutically acceptable salt of  claim 7 , wherein each of R 15a  and R 15b  is independently hydrogen or methyl. 
     
     
         9 . The compound or pharmaceutically acceptable salt of  claim 2 , wherein each of R 16a  and R 16b  is hydrogen. 
     
     
         10 . The compound or pharmaceutically acceptable salt of  claim 2 , wherein   is a single bond, and R 5  is hydrogen or methyl. 
     
     
         11 . The compound or pharmaceutically acceptable salt of  claim 2 , wherein   is a double bond, and R 5  and one of R 6a  and R 6b  is absent. 
     
     
         12 . The compound or pharmaceutically acceptable salt of  claim 2 , wherein R X  is —OH, and R Y  is unsubstituted C 1-3  alkyl. 
     
     
         13 . The compound or pharmaceutically acceptable salt of  claim 2 , wherein n is 1 and R 22  is halogen, —CN, —OR GA , —N(R GA ) 2 , substituted or unsubstituted C 1-6  alkyl, or substituted or unsubstituted C 3-6  carbocylyl, wherein each instance of R GA  is independently hydrogen or substituted or unsubstituted C 1-3  alkyl. 
     
     
         14 . The compound or pharmaceutically acceptable salt of  claim 2 , wherein each of R 1a , R 1b , R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , and R 12b  is hydrogen. 
     
     
         15 . The compound or pharmaceutically acceptable salt of  claim 1 , wherein the compound of Formula (I) is a compound of Formula (I-a) or (I-b): 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof. 
     
     
         16 . The compound or pharmaceutically acceptable salt of  claim 15 , wherein the compound of Formula (I-a) is a compound of Formula (I-c): 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof. 
     
     
         17 . The compound or pharmaceutically acceptable salt of  claim 15 , wherein the compound of Formula (I-b) is a compound of Formula (I-d): 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof. 
     
     
         18 . A compound of Formula (II): 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein
    represents a single or double bond, provided if a double bond is present, then one of R 6a  or R 6b  is absent and R 5  is absent; 
 R X  is selected from the group consisting of halo, —OH, —OR Q1 , and substituted or unsubstituted alkyl, wherein R Q1  is substituted or unsubstituted alkyl; 
 R Y  is halo or substituted or unsubstituted alkyl; or 
 R Y  and R X  may join together with the intervening atoms to form a substituted or unsubstituted carbocyclyl or a substituted or unsubstituted heterocyclyl; 
 R 3  is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; 
 R 5  is hydrogen or methyl; 
 each instance of R 22  is independently selected from the group consisting of halogen, —NO 2 , —CN, —OR GA , —N(R GA ) 2 , —C(═O)R GA , —C(═O)OR GA , —OC(═O)R GA , —OC(═O)OR GA , —C(═O)N(R GA ) 2 , —N(R GA )C(═O)R GA , —OC(═O)N(R GA ) 2 , —N(R GA )C(═O)OR GA , —N(R GA )C(═O)N(R GA ) 2 , —SR GA , —S(═O)R GA , —S(O) 2 R GA , —S(O) 2 OR GA , —OS(O) 2 R GA , —S(═O) 2 N(R GA ) 2 , —N(R GA )S(═O) 2 R GA , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocylyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl, wherein each instance of R GA  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted C 3-6  carbocylyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to oxygen, and a nitrogen protecting group when attached to nitrogen, or two R GA  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclyl or heteroaryl ring; 
 each of R 1a , R 1b , R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 1i a, R 1l b R 12a , and R 12b  is independently selected from the group consisting of hydrogen, halogen, cyano, —NO 2 , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR A1 , —N(R A1 ) 2 , —SR A1 , —C(═O)R A1 , —C(═O)OR A1 , —C(═O)SR A1 , —C(═O)N(R A1 ) 2 , —OC(═O)R A1 , —OC(═O)OR A1 , —OC(═O)N(R A1 ) 2 , —OC(═O)SR A1 , —OS(═O) 2 R A1 , —OS(═O) 2 OR A1 , —OS(═O) 2 N(R A1 ) 2 , —N(R A1 )C(═O)R A1 , —N(R A1 )C(═NR A1 )R A1 , —N(R A1 )C(═O)OR A1 , —N(R A1 )C(═O)N(R A1 ) 2 , —N(R A1 )S(═O) 2 R A1 , —N(R A1 )C(═NR A1 )N(R A1 ) 2 , —N(R A1 )S(═O) 2 OR A1 , —N(R A1 )S(═O) 2 N(R A1 ) 2 , —SC(═O)OR A1 , —SC(═O)R A1 , —SC(═O)SR A1 , —SC(═O)N(R A1 ) 2 , —S(═O) 2 R A1 , —S(═O) 2 OR A1 , or —S(═O) 2 N(R A1 ) 2 , wherein each instance of R A1  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted C 3-6  carbocyclyl, or substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to oxygen, a nitrogen protecting group when attached to nitrogen, and a sulfur protecting group when attached to sulfur, or two R A1  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclic ring; 
 each of R 6a  and R 6b  is independently selected from the group consisting of hydrogen, halogen, cyano, —NO 2 , —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, and substituted or unsubstituted alkynyl; or R 6a  and R 6b  are joined to form an oxo (═O) group; 
 each of R 15a , R 15b , R 16a , and R 16b  is independently selected from the group consisting of hydrogen, halogen, —CN, —NO 2 , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR C3 , —N(R C3 ) 2 , —SR C3 , —C(═O)R C3 , —C(═O)OR C3 , —C(═O)SR C3 , —C(═O)N(R C3 ) 2 , —OC(═O)R C3 , —OC(═O)OR C3 , —OC(═O)N(R C3 ) 2 , —OC(═O)SR C3 , —OS(═O) 2 R C3 , —OS(═O) 2 OR C3 , —OS(═O) 2 N(R C3 ) 2 , —N(R C3 )C(═O)R C3 , —N(R C3 )C(═NR C3 )R C3 , —N(R C3 )C(═O)OR C3 , —N(R C3 )C(═O)N(R C3 ) 2 , —N(R C3 )C(═NR C3 )N(R C3 ) 2 , —N(R C3 )S(═O) 2 R C3 , —N(R C3 )S(═O) 2 OR C3 , —N(R C3 )S(═O) 2 N(R C3 ) 2 , —SC(═O)R C3 , —SC(═O)OR C3 , —SC(═O)SR C3 , —SC(═O)N(R C3 ) 2 , —S(═O) 2 R C3 , —S(═O) 2 OR C3 , or —S(═O) 2 N(R C3 ) 2 , wherein each instance of R C3  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group when attached to oxygen, a nitrogen protecting group when attached to nitrogen, and a sulfur protecting group when attached to sulfur, or two R C3  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclic ring; 
 R 19  is hydrogen or substituted or unsubstituted alkyl; 
 R 18  is substituted or unsubstituted alkyl; and 
 n is 0, 1, 2, or 3; 
 
       provided that when R 5  is hydrogen, R 18  is not —CH 3 . 
     
     
         19 . The compound or pharmaceutically acceptable salt of  claim 18 , wherein each of R 1a , R 1b , R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , and R 12b  is hydrogen. 
     
     
         20 . The compound or pharmaceutically acceptable salt of  claim 18 , wherein R X  is —OH, and R Y  is unsubstituted C 1-3  alkyl. 
     
     
         21 . The compound or pharmaceutically acceptable salt of  claim 19 , wherein n is 1 and R 22  is halogen, —CN, —OR GA , —N(R GA ) 2 , substituted or unsubstituted C 1-6  alkyl, or substituted or unsubstituted C 3-6  carbocylyl, wherein each instance of R GA  is independently hydrogen or substituted or unsubstituted C 1-3  alkyl. 
     
     
         22 . The compound or pharmaceutically acceptable salt of  claim 18 , wherein the compound of Formula (II) is a compound of Formula (IIIa) or (IIIb) 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof. 
     
     
         23 . A compound of Formula (V): 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein
    represents a single or double bond, provided if a double bond is present, then one of R 6a  or R 6b  is absent and R 5  is absent;
 R X  is selected from the group consisting of halo, —OH, —OR Q1 , and substituted or unsubstituted alkyl, wherein R Q1  is substituted or unsubstituted alkyl; 
 R Y  is halo or substituted or unsubstituted alkyl; or 
 R Y  and R X  may join together with the intervening atoms to form a substituted or unsubstituted carbocyclyl or a substituted or unsubstituted heterocyclyl; 
 R 3  is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; 
 R 5  is hydrogen or methyl; 
 each instance of R 22  is independently selected from the group consisting of halogen, —NO 2 , —CN, —OR GA , —N(R GA ) 2 , —C(═O)R GA , —C(═O)OR GA , —OC(═O)R GA , —OC(═O)OR GA , —C(═O)N(R GA ) 2 , —N(R GA )C(═O)R GA , —OC(═O)N(R GA ) 2 , —N(R GA )C(═O)OR GA , —N(R GA )C(═O)N(R GA ) 2 , —SR GA , —S(═O)R GA , —S(O) 2 R GA , —S(O) 2 OR GA , —OS(═O) 2 R GA , —S(═O) 2 N(R GA ) 2 , —N(R GA )S(═O) 2 R GA  substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocylyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl, wherein each instance of R GA  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted C 3-6  carbocylyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to oxygen, and a nitrogen protecting group when attached to nitrogen, or two R GA  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclyl or heteroaryl ring; 
 each of R 1a , R 1b , R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , and R 12b  is independently selected from the group consisting of hydrogen, halogen, cyano, —NO 2 , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR A1 , —N(R A1 ) 2 , —SR A1 , —C(═O)R A1 , —C(═O)OR A1 , —C(═O)SR A1 , —C(═O)N(R A1 ) 2 , —OC(═O)R A1 , —OC(═O)OR A1 , —OC(═O)N(R A1 ) 2 , —OC(═O)SR A1 , —OS(═O) 2 R A1 , —OS(═O) 2 OR A1 , —OS(═O) 2 N(R A1 ) 2 , —N(R A1 )C(═O)R A1 , —N(R A1 )C(═NR A1 )R A1 , —N(R A1 )C(═O)OR A1 , —N(R A1 )C(═O)N(R A1 ) 2 , —N(R A1 )S(═O) 2 R A1 , —N(R A1 )C(═NR A1 )N(R A1 ) 2 , —N(R A1 )S(═O) 2 OR A1 , —N(R A1 )S(═O) 2 N(R A1 ) 2 , —SC(═O)OR A1 , —SC(═O)R A1 , —SC(═O)SR A1 , —SC(═O)N(R A1 ) 2 , —S(═O) 2 R A1 , —S(═O) 2 OR A1 , or —S(═O) 2 N(R A1 ) 2 , wherein each instance of R A1  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted C 3-6  carbocyclyl, or substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to oxygen, a nitrogen protecting group when attached to nitrogen, and a sulfur protecting group when attached to sulfur, or two R A1  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclic ring; 
 each of R 6a  and R 6b  is independently selected from the group consisting of hydrogen, halogen, cyano, —NO 2 , —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, and substituted or unsubstituted alkynyl; or R 6a  and R 6b  are joined to form an oxo (═O) group; 
 each of R 15a , R 15b , R 16a , and R 16b  is independently selected from the group consisting of hydrogen, halogen, —CN, —NO 2 , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR C3 , —N(R C3 ) 2 , —SR C3 , —C(═O)R C3 , —C(═O)OR C3 , —C(═O)SR C3 , —C(═O)N(R C3 ) 2 , —OC(═O)R C3 , —OC(═O)OR C3 , —OC(═O)N(R C3 ) 2 , —OC(═O)SR C3 , —OS(═O) 2 R C3 , —OS(═O) 2 OR C3 , —OS(═O) 2 N(R C3 ) 2 , —N(R C3 )C(═O)R C3 , —N(R C3 )C(═NR C3 )R C3 , —N(R C3 )C(═O)OR C3 , —N(R C3 )C(═O)N(R C3 ) 2 , —N(R C3 )C(═NR C3 )N(R C3 ) 2 , —N(R C3 )S(═O) 2 R C3 , —N(R C3 )S(═O) 2 OR C3 , —N(R C3 )S(═O) 2 N(R C3 ) 2 , —SC(═O)R C3 , —SC(═O)OR C3 , —SC(═O)SR C3 , —SC(═O)N(R C3 ) 2 , —S(═O) 2 R C3 , —S(═O) 2 OR C3 , or —S(═O) 2 N(R C3 ) 2 , wherein each instance of R C3  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group when attached to oxygen, a nitrogen protecting group when attached to nitrogen, and a sulfur protecting group when attached to sulfur, or two R C3  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclic ring; 
 R 19  is hydrogen or substituted or unsubstituted alkyl; and 
 n is 0, 1, 2, or 3. 
 
 
     
     
         24 . A compound of Formula (VIa) 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein
    represents a single or double bond, provided if a double bond is present, then one of R 6a  or R 6b  is absent and R 5  is absent;
 R X  is selected from the group consisting of halo, —OH, —OR Q1 , and substituted or unsubstituted alkyl, wherein R Q1  is substituted or unsubstituted alkyl; 
 R Y  is halo or substituted or unsubstituted alkyl; or 
 R Y  and R X  may join together with the intervening atoms to form a substituted or unsubstituted carbocyclyl or a substituted or unsubstituted heterocyclyl; 
 R 3  is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; 
 R 5  is hydrogen or methyl; 
 each instance of R 22  is independently selected from the group consisting of halogen, —NO 2 , —CN, —OR GA , —N(R GA ) 2 , —C(═O)R GA , —C(═O)OR GA , —OC(═O)R GA , —OC(═O)OR GA , —C(═O)N(R GA ) 2 , —N(R GA )C(═O)R GA , —OC(═O)N(R GA ) 2 , —N(R GA )C(═O)OR GA , —N(R GA )C(═O)N(R GA ) 2 , —SR GA , —S(═O)R GA , —S(O) 2 R GA , —S(O) 2 OR GA , —OS(═O) 2 R GA , —S(═O) 2 N(R GA ) 2 , —N(R GA )S(═O) 2 R GA , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocylyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl, wherein each instance of R GA  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted C 3-6  carbocylyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to oxygen, and a nitrogen protecting group when attached to nitrogen, or two R GA  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclyl or heteroaryl ring; 
 each of R 1a , R 1b , R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , and R 12b  is independently selected from the group consisting of hydrogen, halogen, cyano, —NO 2 , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR A1 , —N(R A1 ) 2 , —SR A1 , —C(═O)R A1 , —C(═O)OR A1 , —C(═O)SR A1 , —C(═O)N(R A1 ) 2 , —OC(═O)R A1 , —OC(═O)OR A1 , —OC(═O)N(R A1 ) 2 , —OC(═O)SR A1 , —OS(═O) 2 R A1 , —OS(═O) 2 OR A1 , —OS(═O) 2 N(R A1 ) 2 , —N(R A1 )C(═O)R A1 , —N(R A1 )C(═NR A1 )R A1 , —N(R A1 )C(═O)OR A1 , —N(R A1 )C(═O)N(R A1 ) 2 , —N(R A1 )S(═O) 2 R A1 , —N(R A1 )C(═NR A1 )N(R A1 ) 2 , —N(R A1 )S(═O) 2 OR A1 , —N(R A1 )S(═O) 2 N(R A1 ) 2 , —SC(═O)OR A1 , —SC(═O)R A1 , —SC(═O)SR A1 , —SC(═O)N(R A1 ) 2 , —S(═O) 2 R A1 , —S(═O) 2 OR A1 , or —S(═O) 2 N(R A1 ) 2 , wherein each instance of R A1  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted C 3-6  carbocyclyl, or substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to oxygen, a nitrogen protecting group when attached to nitrogen, and a sulfur protecting group when attached to sulfur, or two R A1  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclic ring; 
 each of R 6a  and R 6b  is independently selected from the group consisting of hydrogen, halogen, cyano, —NO 2 , —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, and substituted or unsubstituted alkynyl; or R 6a  and R 6b  are joined to form an oxo (═O) group; 
 each of R 5a , R 15b , R 16a , and R 16b  is independently selected from the group consisting of hydrogen, halogen, —CN, —NO 2 , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR C3 , —N(R C3 ) 2 , —SR C3 , —C(═O)R C3 , —C(═O)OR C3 , —C(═O)SR C3 , —C(═O)N(R C3 ) 2 , —OC(═O)R C3 , —OC(═O)OR C3 , —OC(═O)N(R C3 ) 2 , —OC(═O)SR C3 , —OS(═O) 2 R C3 , —OS(═O) 2 OR C3 , —OS(═O) 2 N(R C3 ) 2 , —N(R C3 )C(═O)R C3 , —N(R C3 )C(═NR C3 )R C3 , —N(R C3 )C(═O)OR C3 , —N(R C3 )C(═O)N(R C3 ) 2 , —N(R C3 )C(═NR C3 )N(R C3 ) 2 , —N(R C3 )S(═O) 2 R C3 , —N(R C3 )S(═O) 2 OR C3 , —N(R C3 )S(═O) 2 N(R C3 ) 2 , —SC(═O)R C3 , —SC(═O)OR C3 , —SC(═O)SR C3 , —SC(═O)N(R C3 ) 2 , —S(═O) 2 R C3 , —S(═O) 2 OR C3 , or —S(═O) 2 N(R C3 ) 2 , wherein each instance of R C3  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group when attached to oxygen, a nitrogen protecting group when attached to nitrogen, and a sulfur protecting group when attached to sulfur, or two R C3  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclic ring; 
 R 19  is hydrogen or substituted or unsubstituted alkyl; 
 r is 2 or 3; and 
 n is 0, 1, 2, or 3. 
 
 
     
     
         25 . The compound or pharmaceutically acceptable salt of  claim 24 , wherein R 3  is substituted or unsubstituted C 1-6  alkyl. 
     
     
         26 . The compound or pharmaceutically acceptable salt of  claim 25 , wherein R 3  is C 1-3  alkyl optionally substituted with C 1-3  alkoxy. 
     
     
         27 . The compound or pharmaceutically acceptable salt of  claim 25 , wherein R 3  is methyl, ethyl, n-propyl, —CH 2 OCH 3 , or —CH 2 OCH 2 CH 3 . 
     
     
         28 . The compound or pharmaceutically acceptable salt of  claim 24 , wherein R 19  is hydrogen or unsubstituted C 1-3  alkyl. 
     
     
         29 . The compound or pharmaceutically acceptable salt of  claim 24 , wherein each of R 15  and R 15b  is independently hydrogen or substituted or unsubstituted alkyl. 
     
     
         30 . The compound or pharmaceutically acceptable salt of  claim 29 , wherein each of R 1a  and R 15b  is independently hydrogen or methyl. 
     
     
         31 . The compound or pharmaceutically acceptable salt of  claim 24 , wherein each of R 16a  and R 16b  is hydrogen. 
     
     
         32 . The compound or pharmaceutically acceptable salt of  claim 24 , wherein   is a single bond, and R 5  is hydrogen or methyl. 
     
     
         33 . The compound or pharmaceutically acceptable salt of  claim 24 , wherein   is a double bond, and R 5  and one of R 6a  and R 6b  is absent. 
     
     
         34 . The compound or pharmaceutically acceptable salt of  claim 24 , wherein R X  is —OH, and R Y  is unsubstituted C 1-3  alkyl. 
     
     
         35 . The compound or pharmaceutically acceptable salt of  claim 24 , wherein n is 1 and R 22  is halogen, —CN, —OR GA , —N(R GA ) 2 , substituted or unsubstituted C 1-6  alkyl, or substituted or unsubstituted C 3-6  carbocylyl, wherein each instance of R GA  is independently hydrogen or substituted or unsubstituted C 1-3  alkyl. 
     
     
         36 . The compound or pharmaceutically acceptable salt of  claim 24 , wherein the compound of Formula (VIa) is a compound of Formula (VIa-a): 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof. 
     
     
         37 . The compound or pharmaceutically acceptable salt of  claim 36 , wherein the compound of Formula (VIa-a) is a compound of Formula (VIa-b): 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof. 
     
     
         38 . The compound or pharmaceutically acceptable salt of  claim 36 , wherein the compound of Formula (VIa-b) is a compound of Formula (VIa-c) or (VIa-d): 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof. 
     
     
         39 . The compound or pharmaceutically acceptable salt of  claim 24 , wherein the compound of Formula (VIa) is a compound of Formula (VIa-e): 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof. 
     
     
         40 . A compound of Formula (VIb) 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein
    represents a single or double bond, provided if a double bond is present, then one of R 6a  or R 6b  is absent and R 5  is absent;
 R X  is selected from the group consisting of halo, —OH, —OR Q1 , and substituted or unsubstituted alkyl, wherein R Q1  is substituted or unsubstituted alkyl; 
 R Y  is halo or substituted or unsubstituted alkyl; or 
 R Y  and R X  may join together with the intervening atoms to form a substituted or unsubstituted carbocyclyl or a substituted or unsubstituted heterocyclyl; 
 R 3  is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; 
 R 5  is hydrogen or methyl; 
 each instance of R 22  is independently selected from the group consisting of halogen, —NO 2 , —CN, —OR GA , —N(R GA ) 2 , —C(═O)R GA , —C(═O)OR GA , —OC(═O)R GA , —OC(═O)OR GA , —C(═O)N(R GA ) 2 , —N(R GA )C(═O)R GA , —OC(═O)N(R GA ) 2 , —N(R GA )C(═O)OR GA , —N(R GA )C(═O)N(R GA ) 2 , —SR GA , —S(═O)R GA , —S(O) 2 R GA , —S(O) 2 OR GA , —OS(═O) 2 R GA , —S(═O) 2 N(R GA ) 2 , —N(R GA )S(═O) 2 R GA  substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocylyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl, wherein each instance of R GA  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted C 3-6  carbocylyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to oxygen, and a nitrogen protecting group when attached to nitrogen, or two R GA  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclyl or heteroaryl ring; 
 each of R 1a , R 1b , R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , and R 12b  is independently selected from the group consisting of hydrogen, halogen, cyano, —NO 2 , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR A1 , —N(R A1 ) 2 , —SR A1 , —C(═O)R A1 , —C(═O)OR A1 , —C(═O)SR A1 , —C(═O)N(R A1 ) 2 , —OC(═O)R A1 , —OC(═O)OR A1 , —OC(═O)N(R A1 ) 2 , —OC(═O)SR A1 , —OS(═O) 2 R A1 , —OS(═O) 2 OR A1 , —OS(═O) 2 N(R A1 ) 2 , —N(R A1 )C(═O)R A1 , —N(R A1 )C(═NR A1 )R A1 , —N(R A1 )C(═O)OR A1 , —N(R A1 )C(═O)N(R A1 ) 2 , —N(R A1 )S(═O) 2 R A1 , —N(R A1 )C(═NR A1 )N(R A1 ) 2 , —N(R A1 )S(═O) 2 OR A1 , —N(R A1 )S(═O) 2 N(R A1 ) 2 , —SC(═O)OR A1 , —SC(═O)R A1 , —SC(═O)SR A1 , —SC(═O)N(R A1 ) 2 , —S(═O) 2 R A1 , —S(═O) 2 OR A1 , or —S(═O) 2 N(R A1 ) 2 , wherein each instance of R A1  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted C 3-6  carbocyclyl, or substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to oxygen, a nitrogen protecting group when attached to nitrogen, and a sulfur protecting group when attached to sulfur, or two R A1  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclic ring; 
 each of R 6a  and R 6b  is independently selected from the group consisting of hydrogen, halogen, cyano, —NO 2 , —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, and substituted or unsubstituted alkynyl; or R 6a  and R 6b  are joined to form an oxo (═O) group; 
 each of R 15a , R 15b , R 16a , and R 16b  is independently selected from the group consisting of hydrogen, halogen, —CN, —NO 2 , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR C3 , —N(R C3 ) 2 , —SR C3 , —C(═O)R C3 , —C(═O)OR C3 , —C(═O)SR C3 , —C(═O)N(R C3 ) 2 , —OC(═O)R C3 , —OC(═O)OR C3 , —OC(═O)N(R C3 ) 2 , —OC(═O)SR C3 , —OS(═O) 2 R C3 , —OS(═O) 2 OR C3 , —OS(═O) 2 N(R C3 ) 2 , —N(R C3 )C(═O)R C3 , —N(R C3 )C(═NR C3 )R C3 , —N(R C3 )C(═O)OR C3 , —N(R C3 )C(═O)N(R C3 ) 2 , —N(R C3 )C(═NR C3 )N(R C3 ) 2 , —N(R C3 )S(═O) 2 R C3 , —N(R C3 )S(═O) 2 OR C3 , —N(R C3 )S(═O) 2 N(R C3 ) 2 , —SC(═O)R C3 , —SC(═O)OR C3 , —SC(═O)SR C3 , —SC(═O)N(R C3 ) 2 , —S(═O) 2 R C3 , —S(═O) 2 OR C3 , or —S(═O) 2 N(R C3 ) 2 , wherein each instance of R C3  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group when attached to oxygen, a nitrogen protecting group when attached to nitrogen, and a sulfur protecting group when attached to sulfur, or two R C3  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclic ring; 
 R 19  is hydrogen or substituted or unsubstituted alkyl; 
 p is 2 or 3; and 
 n is 0, 1, 2, or 3. 
 
 
     
     
         41 . The compound or pharmaceutically acceptable salt of  claim 40 , wherein R 3  is substituted or unsubstituted C 1-6  alkyl. 
     
     
         42 . The compound or pharmaceutically acceptable salt of  claim 41 , wherein R 3  is C 1-3  alkyl optionally substituted with C 1-3  alkoxy. 
     
     
         43 . The compound or pharmaceutically acceptable salt of  claim 42 , wherein R 3  is methyl, ethyl, n-propyl, —CH 2 OCH 3 , or —CH 2 OCH 2 CH 3 . 
     
     
         44 . The compound or pharmaceutically acceptable salt of  claim 40 , wherein R 19  is hydrogen or unsubstituted C 1-3  alkyl. 
     
     
         45 . The compound or pharmaceutically acceptable salt of  claim 40 , wherein each of R 15a  and R 15b  is independently hydrogen or substituted or unsubstituted alkyl. 
     
     
         46 . The compound or pharmaceutically acceptable salt of  claim 45 , wherein each of R 15a  and R 15b  is independently hydrogen or methyl. 
     
     
         47 . The compound or pharmaceutically acceptable salt of  claim 40 , wherein each of R 16a  and R 16b  is hydrogen. 
     
     
         48 . The compound or pharmaceutically acceptable salt of  claim 40 , wherein   is a single bond, and R 5  is hydrogen or methyl. 
     
     
         49 . The compound or pharmaceutically acceptable salt of  claim 40 , wherein   is a double bond, and R 5  and one of R 6a  and R 6b  is absent. 
     
     
         50 . The compound or pharmaceutically acceptable salt of  claim 40 , wherein R X  is —OH, and R Y  is unsubstituted C 1-3  alkyl. 
     
     
         51 . The compound or pharmaceutically acceptable salt of  claim 40 , wherein n is 1 and R 22  is halogen, —CN, —OR GA , —N(R GA ) 2 , substituted or unsubstituted C 1-6  alkyl, or substituted or unsubstituted C 3-6  carbocylyl, wherein each instance of R GA  is independently hydrogen or substituted or unsubstituted C 1-3  alkyl. 
     
     
         52 . The compound or pharmaceutically acceptable salt of  claim 40 , wherein the compound of Formula (VIb) is a compound of Formula (VIb-b): 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof. 
     
     
         53 . The compound or pharmaceutically acceptable salt of  claim 52 , wherein the compound of Formula (VIb-b) is a compound of Formula (VIb-c) or (VIb-d): 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof. 
     
     
         54 . The compound or pharmaceutically acceptable salt of  claim 40 , wherein the compound of Formula (VIb) is a compound of Formula (VIb-e): 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof. 
     
     
         55 . A compound of Formula (VII) 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein
    represents a single or double bond, provided if a double bond is present, then one of R 6a  or R 6b  is absent and R 5  is absent;
 R X  is selected from the group consisting of halo, —OH, —OR G1 , and substituted or unsubstituted alkyl, wherein R G1  is substituted or unsubstituted alkyl; 
 R is halo or substituted or unsubstituted alkyl; or 
 R Y  and R X  may join together with the intervening atoms to form a substituted or unsubstituted carbocyclyl or a substituted or unsubstituted heterocyclyl; 
 R 3  is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; 
 R 5  is hydrogen or methyl; 
 each instance of R 22  is independently selected from the group consisting of halogen, —NO 2 , —CN, —OR GA , —N(R GA ) 2 , —C(═O)R GA , —C(═O)OR GA , —OC(═O)R GA , —OC(═O)OR GA , —C(═O)N(R GA ) 2 , —N(R GA )C(═O)R GA , —OC(═O)N(R GA ) 2 , —N(R GA )C(═O)OR GA , —N(R GA )C(═O)N(R GA ) 2 , —SR GA , —S(═O)R GA , —S(O) 2 R GA , —S(O) 2 OR GA , —OS(O) 2 R GA , —S(═O) 2 N(R GA ) 2 , —N(R GA )S(═O) 2 R GA , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocylyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl, wherein each instance of R GA  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted C 3-6  carbocylyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to oxygen, and a nitrogen protecting group when attached to nitrogen, or two R GA  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclyl or heteroaryl ring; 
 each of R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 1a , R 11b , R 12a , and R 12b  is independently selected from the group consisting of hydrogen, halogen, cyano, —NO 2 , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR A 1, —N(R A1 ) 2 , —SR A1 , —C(═O)R A1 , —C(═O)OR A1 , —C(═O)SR A1 , —C(═O)N(R A1 ) 2 , —OC(═O)R A1 , —OC(═O)OR A1 , —OC(═O)N(R A1 ) 2 , —OC(═O)SR A1 , —OS(═O) 2 R A1 , —OS(═O) 2 OR A1 , —OS(═O) 2 N(R A1 ) 2 , —N(R A1 )C(═O)R A1 , —N(R A1 )C(═NR A1 )R A1 , —N(R A1 )C(═O)OR A1 , —N(R A1 )C(═O)N(R A1 ) 2 , —N(R A1 )S(═O) 2 R A1 , —N(R A1 )C(═NR A1 )N(R A1 ) 2 , —N(R A1 )S(═O) 2 OR A1 , —N(R A1 )S(═O) 2 N(R A1 ) 2 , —SC(═O)OR A1 , —SC(═O)R A1 , —SC(═O)SR A1 , —SC(═O)N(R A1 ) 2 , —S(═O) 2 R A1 , —S(═O) 2 OR A1 , or —S(═O) 2 N(R A1 ) 2 , wherein each instance of R A1  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted C 3-6  carbocyclyl, or substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to oxygen, a nitrogen protecting group when attached to nitrogen, and a sulfur protecting group when attached to sulfur, or two R A1  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclic ring; 
 each of R 6a  and R 6b  is independently selected from the group consisting of hydrogen, halogen, cyano, —NO 2 , —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, and substituted or unsubstituted alkynyl; or R 6a  and R 6b  are joined to form an oxo (═O) group; 
 each of Ra R 15b , R 16a , and R 16b  is independently selected from the group consisting of hydrogen, halogen, —CN, —NO 2 , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR C3 , —N(R C3 ) 2 , —SR C3 , —C(═O)R C3 , —C(═O)OR C3 , —C(═O)SR C3 , —C(═O)N(R C3 ) 2 , —OC(═O)R C3 , —OC(═O)OR C3 , —OC(═O)N(R C3 ) 2 , —OC(═O)SR C3 , —OS(═O) 2 R C3 , —OS(═O) 2 OR C3 , —OS(═O) 2 N(R C3 ) 2 , —N(R C3 )C(═O)R C3 , —N(R C3 )C(═NR C3 )R C3 , —N(R C3 )C(═O)OR C3 , —N(R C3 )C(═O)N(R C3 ) 2 , —N(R C3 )C(═NR C3 )N(R C3 ) 2 , —N(R C3 )S(═O) 2 R C3 , —N(R C3 )S(═O) 2 OR C3 , —N(R C3 )S(═O) 2 N(R C3 ) 2 , —SC(═O)R C3 , —SC(═O)OR C3 , —SC(═O)SR C3 , —SC(═O)N(R C3 ) 2 , —S(═O) 2 R C3 , —S(═O) 2 OR C3 , or —S(═O) 2 N(R C3 ) 2 , wherein each instance of R C3  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group when attached to oxygen, a nitrogen protecting group when attached to nitrogen, and a sulfur protecting group when attached to sulfur, or two R C3  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclic ring; 
 R 19  is hydrogen or substituted or unsubstituted alkyl; and 
 n is 0, 1, 2, or 3. 
 
 
     
     
         56 . The compound or pharmaceutically acceptable salt of  claim 55 , wherein R 3  is substituted or unsubstituted C 1-6  alkyl. 
     
     
         57 . The compound or pharmaceutically acceptable salt of  claim 56 , wherein R 3  is C 1-3  alkyl optionally substituted with C 1-3  alkoxy. 
     
     
         58 . The compound or pharmaceutically acceptable salt of  claim 57 , wherein R 3  is methyl, ethyl, n-propyl, —CH 2 OCH 3 , or —CH 2 OCH 2 CH 3 . 
     
     
         59 . The compound or pharmaceutically acceptable salt of  claim 55 , wherein R 19  is hydrogen or unsubstituted C 1-3  alkyl. 
     
     
         60 . The compound or pharmaceutically acceptable salt of  claim 55 , wherein each of R 15a  and R 15b  is independently hydrogen or substituted or unsubstituted alkyl. 
     
     
         61 . The compound or pharmaceutically acceptable salt of  claim 60 , wherein each of R 15a  and R 15b  is independently hydrogen or methyl. 
     
     
         62 . The compound or pharmaceutically acceptable salt of  claim 55 , wherein each of R 16a  and R 16b  is hydrogen. 
     
     
         63 . The compound or pharmaceutically acceptable salt of  claim 55 , wherein   is a single bond, and R 5  is hydrogen or methyl. 
     
     
         64 . The compound or pharmaceutically acceptable salt of  claim 55 , wherein   is a double bond, and R 5  and one of R 6a  and R 6b  is absent. 
     
     
         65 . The compound or pharmaceutically acceptable salt of  claim 55 , wherein R X  is —OH, and R Y  is unsubstituted C 1-3  alkyl. 
     
     
         66 . The compound or pharmaceutically acceptable salt of  claim 55 , wherein n is 1 and R 22  is halogen, —CN, —OR GA , —N(R GA ) 2 , substituted or unsubstituted C 1-6  alkyl, or substituted or unsubstituted C 3-6  carbocylyl, wherein each instance of R GA  is independently hydrogen or substituted or unsubstituted C 1-3  alkyl. 
     
     
         67 . The compound or pharmaceutically acceptable salt of  claim 55 , wherein the compound of Formula (VII) is a compound of Formula (VII-b) 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof. 
     
     
         68 . The compound or pharmaceutically acceptable salt of  claim 67 , wherein the compound of Formula (VII-b) is a compound of Formula (VII-c): 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof. 
     
     
         69 . A compound of Formula (VIII): 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein
    represents a single or double bond, provided if a double bond is present, then one of R 6a  or R 6b  is absent and R 5  is absent;
 R X  is selected from the group consisting of halo, —OH, —OR Q1 , and substituted or unsubstituted alkyl, wherein R Q1  is substituted or unsubstituted alkyl; 
 R Y  is halo or substituted or unsubstituted alkyl; or 
 R Y  and R X  may join together with the intervening atoms to form a substituted or unsubstituted carbocyclyl or a substituted or unsubstituted heterocyclyl; 
 R 3  is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; 
 R 5  is hydrogen or methyl; 
 each instance of R 22  is independently selected from the group consisting of halogen, —NO 2 , —CN, —OR GA , —N(R GA ) 2 , —C(═O)R GA , —C(═O)OR GA , —OC(═O)R GA , —OC(═O)OR GA , —C(═O)N(R GA ) 2 , —N(R GA )C(═O)R GA , —OC(═O)N(R GA ) 2 , —N(R GA )C(═O)OR GA , —N(R GA )C(═O)N(R GA ) 2 , —SR GA , —S(═O)R GA , —S(O) 2 R GA , —S(O) 2 OR GA , —OS(═O) 2 R GA , —S(═O) 2 N(R GA ) 2 , —N(R GA )S(═O) 2 R GA , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocylyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl, wherein each instance of R GA  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted C 3-6  carbocylyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to oxygen, and a nitrogen protecting group when attached to nitrogen, or two R GA  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclyl or heteroaryl ring; 
 each of R 1a , R 1b , R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , and R 12b  is independently selected from the group consisting of hydrogen, halogen, cyano, —NO 2 , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR A1 , —N(R A1 ) 2 , —SR A 1, —C(═O)R A1 , —C(═O)OR A1 , —C(═O)SR A1 , —C(═O)N(R A1 ) 2 , —OC(═O)R A1 , —OC(═O)OR A1 , —OC(═O)N(R A1 ) 2 , —OC(═O)SR A1 , —OS(═O) 2 R A1 , —OS(═O) 2 OR A1 , —OS(═O) 2 N(R A1 ) 2 , —N(R A1 )C(═O)R A1 , —N(R A1 )C(═NR A1 )R A1 , —N(R A1 )C(═O)OR A1 , —N(R A1 )C(═O)N(R A1 ) 2 , —N(R A1 )S(═O) 2 R A1 , —N(R A1 )C(═NR A1 )N(R A1 ) 2 , —N(R A1 )S(═O) 2 OR A1 , —N(R A1 )S(═O) 2 N(R A1 ) 2 , —SC(═O)OR A1 , —SC(═O)R A1 , —SC(═O)SR A1 , —SC(═O)N(R A1 ) 2 , —S(═O) 2 R A1 , —S(═O) 2 OR A1 , or —S(═O) 2 N(R A1 ) 2 , wherein each instance of R A1  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted C 3-6  carbocyclyl, or substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to oxygen, a nitrogen protecting group when attached to nitrogen, and a sulfur protecting group when attached to sulfur, or two R A1  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclic ring; 
 each of R 6a  and R 6b  is independently selected from the group consisting of hydrogen, halogen, cyano, —NO 2 , —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, and substituted or unsubstituted alkynyl; or R 6a  and R 6b  are joined to form an oxo (═O) group; 
 each of R 15a , R 15b , R 16a , and R 16b  is independently selected from the group consisting of hydrogen, halogen, —CN, —NO 2 , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR C3 , —N(R C3 ) 2 , —SR C3 , —C(═O)R C3 , —C(═O)OR C3 , —C(═O)SR C3 , —C(═O)N(R C3 ) 2 , —OC(═O)R C3 , —OC(═O)OR C3 , —OC(═O)N(R C3 ) 2 , —OC(═O)SR C3 , —OS(═O) 2 R C3 , —OS(═O) 2 OR C3 , —OS(═O) 2 N(R C3 ) 2 , —N(R C3 )C(═O)R C3 , —N(R C3 )C(═NR C3 )R C3 , —N(R C3 )C(═O)OR C3 , —N(R C3 )C(═O)N(R C3 ) 2 , —N(R C3 )C(═NR C3 )N(R C3 ) 2 , —N(R C3 )S(═O) 2 R C3 , —N(R C3 )S(═O) 2 OR C3 , —N(R C3 )S(═O) 2 N(R C3 ) 2 , —SC(═O)R C3 , —SC(═O)OR C3 , —SC(═O)SR C3 , —SC(═O)N(R C3 ) 2 , —S(═O) 2 R C3 , —S(═O) 2 OR C3 , or —S(═O) 2 N(R C3 ) 2 , wherein each instance of R C3  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group when attached to oxygen, a nitrogen protecting group when attached to nitrogen, and a sulfur protecting group when attached to sulfur, or two R C3  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclic ring; 
 R 19  is hydrogen or substituted or unsubstituted alkyl; 
 s is 2; and 
 n is 0, 1, 2, or 3. 
 
 
     
     
         70 . A compound of Formula (IX): 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein
 R X  is selected from the group consisting of halo, —OH, —OR Q1 , and substituted or unsubstituted alkyl, wherein R Q1  is substituted or unsubstituted alkyl; 
 R Y  is halo or substituted or unsubstituted alkyl; or 
 R Y  and R X  may join together with the intervening atoms to form a substituted or unsubstituted carbocyclyl or a substituted or unsubstituted heterocyclyl; 
 R 3  is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; 
 R 5  is hydrogen or methyl; 
 each instance of R 22  is independently selected from the group consisting of halogen, —NO 2 , —CN, —OR GA , —N(R GA ) 2 , —C(═O)R GA , —C(═O)OR GA , —OC(═O)R GA , —OC(═O)OR GA , —C(═O)N(R GA ) 2 , —N(R GA )C(═O)R GA , —OC(═O)N(R GA ) 2 , —N(R GA )C(═O)OR GA , —N(R GA )C(═O)N(R GA ) 2 , —SR GA , —S(═O)R GA , —S(O) 2 R GA , —S(O) 2 OR GA , —OS(═O) 2 R GA , —S(═O) 2 N(R GA ) 2 , —N(R GA )S(═O) 2 R GA  substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocylyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl, wherein each instance of R GA  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted C 3-6  carbocylyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to oxygen, and a nitrogen protecting group when attached to nitrogen, or two R GA  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclyl or heteroaryl ring; 
 each of R 1a , R 1b , R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , and R 12b  is independently selected from the group consisting of hydrogen, halogen, cyano, —NO 2 , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR A1 , —N(R A1 ) 2 , —SR A 1, —C(═O)R A1 , —C(═O)OR A1 , —C(═O)SR A1 , —C(═O)N(R A1 ) 2 , —OC(═O)R A1 , —OC(═O)OR A1 , —OC(═O)N(R A1 ) 2 , —OC(═O)SR A1 , —OS(═O) 2 R A1 , —OS(═O) 2 OR A1 , —OS(═O) 2 N(R A1 ) 2 , —N(R A1 )C(═O)R A1 , —N(R A1 )C(═NR A1 )R A1 , —N(R A1 )C(═O)OR A1 , —N(R A1 )C(═O)N(R A1 ) 2 , —N(R A1 )S(═O) 2 R A1 , —N(R A1 )C(═NR A1 )N(R A1 ) 2 , —N(R A1 )S(═O) 2 OR A1 , —N(R A1 )S(═O) 2 N(R A1 ) 2 , —SC(═O)OR A1 , —SC(═O)R A1 , —SC(═O)SR A1 , —SC(═O)N(R A1 ) 2 , —S(═O) 2 R A1 , —S(═O) 2 OR A1 , or —S(═O) 2 N(R A1 ) 2 , wherein each instance of R A1  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted C 3-6  carbocyclyl, or substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to oxygen, a nitrogen protecting group when attached to nitrogen, and a sulfur protecting group when attached to sulfur, or two R A1  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclic ring; 
 each of R 6a  and R 6b  is independently selected from the group consisting of hydrogen, halogen, cyano, —NO 2 , —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, and substituted or unsubstituted alkynyl; or R 6a  and R 6b  are joined to form an oxo (═O) group; 
 each of R 15a , R 15b , R 16a , and R 16b  is independently selected from the group consisting of hydrogen, halogen, —CN, —NO 2 , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR C3 , —N(R C3 ) 2 , —SR C3 , —C(═O)R C3 , —C(═O)OR C3 , —C(═O)SR C3 , —C(═O)N(R C3 ) 2 , —OC(═O)R C3 , —OC(═O)OR C3 , —OC(═O)N(R C3 ) 2 , —OC(═O)SR C3 , —OS(═O) 2 R C3 , —OS(═O) 2 OR C3 , —OS(═O) 2 N(R C3 ) 2 , —N(R C3 )C(═O)R C3 , —N(R C3 )C(═NR C3 )R C3 , —N(R C3 )C(═O)OR C3 , —N(R C3 )C(═O)N(R C3 ) 2 , —N(R C3 )C(═NR C3 )N(R C3 ) 2 , —N(R C3 )S(═O) 2 R C3 , —N(R C3 )S(═O) 2 OR C3 , —N(R C3 )S(═O) 2 N(R C3 ) 2 , —SC(═O)R C3 , —SC(═O)OR C3 , —SC(═O)SR C3 , —SC(═O)N(R C3 ) 2 , —S(═O) 2 R C3 , —S(═O) 2 OR C3 , or —S(═O) 2 N(R C3 ) 2 , wherein each instance of R C3  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group when attached to oxygen, a nitrogen protecting group when attached to nitrogen, and a sulfur protecting group when attached to sulfur, or two R C3  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclic ring; 
 R 19  is hydrogen or substituted or unsubstituted alkyl; and 
 n is 0, 1, 2, or 3. 
 
     
     
         71 . A compound of Formula (X): 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein
    represents a single or double bond, provided if a double bond is present, then one of R 6a  or R 6b  is absent and R 5  is absent;
 R X  is selected from the group consisting of halo, —OH, —OR Q1 , and substituted or unsubstituted alkyl, wherein R Q1  is substituted or unsubstituted alkyl; 
 R Y  is halo or substituted or unsubstituted alkyl; or 
 R Y  and R X  may join together with the intervening atoms to form a substituted or unsubstituted carbocyclyl or a substituted or unsubstituted heterocyclyl; 
 R 3  is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; 
 R 5  is hydrogen or methyl; 
 each instance of R 22  is independently selected from the group consisting of halogen, —NO 2 , —CN, —OR GA , —N(R GA ) 2 , —C(═O)R GA , —C(═O)OR GA , —OC(═O)R GA , —OC(═O)OR GA , —C(═O)N(R GA ) 2 , —N(R GA )C(═O)R GA , —OC(═O)N(R GA ) 2 , —N(R GA )C(═O)OR GA , —N(R GA )C(═O)N(R GA ) 2 , —SR GA , —S(═O)R GA , —S(O) 2 R GA , —S(O) 2 OR GA , —OS(═O) 2 R GA , —S(═O) 2 N(R GA ) 2 , —N(R GA )S(═O) 2 R GA , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocylyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl, wherein each instance of R GA  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted C 3-6  carbocylyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to oxygen, and a nitrogen protecting group when attached to nitrogen, or two R GA  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclyl or heteroaryl ring; 
 each of R 1a , R 1b , R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , and R 12b  is independently selected from the group consisting of hydrogen, halogen, cyano, —NO 2 , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR A1 , —N(R A1 ) 2 , —SR A 1, —C(═O)R A1 , —C(═O)OR A1 , —C(═O)SR A1 , —C(═O)N(R A1 ) 2 , —OC(═O)R A1 , —OC(═O)OR A1 , —OC(═O)N(R A1 ) 2 , —OC(═O)SR A1 , —OS(═O) 2 R A1 , —OS(═O) 2 OR A1 , —OS(═O) 2 N(R A1 ) 2 , —N(R A1 )C(═O)R A1 , —N(R A1 )C(═NR A1 )R A1 , —N(R A1 )C(═O)OR A1 , —N(R A1 )C(═O)N(R A1 ) 2 , —N(R A1 )S(═O) 2 R A1 , —N(R A1 )C(═NR A1 )N(R A1 ) 2 , —N(R A1 )S(═O) 2 OR A1 , —N(R A1 )S(═O) 2 N(R A1 ) 2 , —SC(═O)OR A1 , —SC(═O)R A1 , —SC(═O)SR A1 , —SC(═O)N(R A1 ) 2 , —S(═O) 2 R A1 , —S(═O) 2 OR A1 , or —S(═O) 2 N(R A1 ) 2 , wherein each instance of R A1  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted C 3-6  carbocyclyl, or substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to oxygen, a nitrogen protecting group when attached to nitrogen, and a sulfur protecting group when attached to sulfur, or two R A1  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclic ring; 
 each of R 6a  and R 6b  is independently selected from the group consisting of hydrogen, halogen, cyano, —NO 2 , —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, and substituted or unsubstituted alkynyl; or R 6a  and R 6b  are joined to form an oxo (═O) group; 
 each of R 15a , R 15b , R 16a , and R 16b  is independently selected from the group consisting of hydrogen, halogen, —CN, —NO 2 , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR C3 , —N(R C3 ) 2 , —SR C3 , —C(═O)R C3 , —C(═O)OR C3 , —C(═O)SR C3 , —C(═O)N(R C3 ) 2 , —OC(═O)R C3 , —OC(═O)OR C3 , —OC(═O)N(R C3 ) 2 , —OC(═O)SR C3 , —OS(═O) 2 R C3 , —OS(═O) 2 OR C3 , —OS(═O) 2 N(R C3 ) 2 , —N(R C3 )C(═O)R C3 , —N(R C3 )C(═NR C3 )R C3 , —N(R C3 )C(═O)OR C3 , —N(R C3 )C(═O)N(R C3 ) 2 , —N(R C3 )C(═NR C3 )N(R C3 ) 2 , —N(R C3 )S(═O) 2 R C3 , —N(R C3 )S(═O) 2 OR C3 , —N(R C3 )S(═O) 2 N(R C3 ) 2 , —SC(═O)R C3 , —SC(═O)OR C3 , —SC(═O)SR C3 , —SC(═O)N(R C3 ) 2 , —S(═O) 2 R C3 , —S(═O) 2 OR C3 , or —S(═O) 2 N(R C3 ) 2 , wherein each instance of R C3  is independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-6  alkyl, substituted or unsubstituted C 2-6  alkenyl, substituted or unsubstituted C 2-6  alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group when attached to oxygen, a nitrogen protecting group when attached to nitrogen, and a sulfur protecting group when attached to sulfur, or two R C3  groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclic ring; 
 R 19  is hydrogen or substituted or unsubstituted alkyl; 
 q is 2; and 
 n is 0, 1, 2, or 3. 
 
 
     
     
         72 . A compound selected from 
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof. 
     
     
         73 . A pharmaceutical composition comprising the compound or pharmaceutically acceptable salt of  claim 1 , and a pharmaceutically acceptable excipient. 
     
     
         74 . A compound selected from 
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
     
     
         75 . A pharmaceutical composition comprising a compound of  claim 74 , and a pharmaceutically acceptable excipient.

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